HLB-0532247 

HLB-0532247 is a cell-permeable phosphoramidate prodrug of 3'-deoxy-3',4'-didehydrocytidine (ddhC). HLB-0532247 increases the intracellular level of the endogenous antiviral nucleotide ddhCTP. HLB-0532247 reduces the titers of Zika virus and West Nile virus in cell cultures. HLB-0532247 can be used in studies related to Zika virus infection, West Nile virus infection, and coronavirus infection^[1][2].

HLB-0532247 (0.1-1.0 mM) potently reduces Zika virus levels by more than 1 log₁₀ pfu/mL at a concentration of 0.1 mM in HUH7 and HUH7.5 cells after 4 days, while it shows weak activity in Vero cells^[1].
HLB-0532247 (1.0 mM) potently reduces West Nile virus levels by more than 4 log₁₀ pfu/mL in HUH7 and HUH7.5 cells, but shows no activity in Vero cells^[1].
HLB-0532247 (1.0 mM; 2-5 days) shows no cytotoxicity in Vero and HUH7 cells after 2 days of treatment, and only exhibits mild toxicity (cell viability >60%) after 5 days of treatment at 1.0 mM, with its CC₅₀ greater than 1 mM^[1].
HLB-0532247 (2 μM; 0-120 min) is stable in plasma, with a remaining proportion of >87% after incubation at 37°C for 2 hours^[1].
HLB-0532247 (2 μM; 0-360 min) shows stable properties in simulated gastric fluid, with approximately 76% remaining after incubation at 37°C for 6 hours^[1].
HLB-0532247 (2-10 μM; 2 h) exhibits a mean apparent permeability coefficient of 0.3 nm/sec in Caco-2 cells, showing cellular permeability similar to that of sofosbuvir^[1].
HLB-0532247 (100 μM; 24 h) is metabolized to ddhCTP in HUH7 cells. After treatment with 100 μM for 24 h, 3.8 nmol of ddhCTP is produced per 5×10⁶ cells (intracellular concentration >1 mM), representing a 29-fold increase compared with cells treated with ddhC^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

494.43

C₂₁H₂₇N₄O₈P

2850362-12-6

NC(C=CN1[C@H]2[C@H](O)C=C(CO[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O)O2)=NC1=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Passow KT, et al. A Chemical Strategy for Intracellular Arming of an Endogenous Broad-Spectrum Antiviral Nucleotide. J Med Chem. 2021;64(20):15429-15439.

  [2]. Zhu M, et al. CMPK2 is a host restriction factor that inhibits infection of multiple coronaviruses in a cell-intrinsic manner. PLoS Biol. 2023;21(3):e3002039. Published 2023 Mar 17.  [Content Brief]